Question 1

Which of the following class of drugs is a common treatment for hypertension?

Accepted Answer

A)  beta blocker 
B)  statins 
C)  protease inhibitors 
D)  phosphodiesterase inhibitors 
E)  None of the answers is correct. 
A)  beta blocker 
B)  statins 
C)  protease inhibitors 
D)  phosphodiesterase inhibitors 
E)  None of the answers is correct. A

Question 2

Describe how certain bacteria can development resistance to penicillin.

Accepted Answer

Some bacteria are resistant to penicillin because they contain β-lactamase enzymes, which hydrolyze the β-lactam ring of penicillin rendering it inactive. Resistance can develop in a population because these resistant organisms will survive due to selection and they overtake other organisms in the population.

Question 3

How is genomic information used to develop new drugs?

Accepted Answer

Genes for related target proteins can be identified by matching similar sequences in the genome information. Mouse models have been used extensively in drug development. Mice with specific target genes knocked out can be studied. If disruption of a gene has a desirable effect, then the product of this gene is a promising drug target.

Question 4

First attempts to develop cholesterol-lowering drugs targeted the later steps in cholesterol biosynthesis. Why did this strategy have to be abandoned?

Accepted Answer

A)  These reactions were so efficient that they could not be blocked. 
B)  The accumulation of an insoluble substrate caused cataracts and other deleterious side effects. 
C)  All of the drugs that were developed actually enhanced cholesterol synthesis. 
D)  None of the drugs that were developed could survive the acid conditions in the stomach. 
E)  These drugs caused untreatable gall stones. 
A)  These reactions were so efficient that they could not be blocked. 
B)  The accumulation of an insoluble substrate caused cataracts and other deleterious side effects. 
C)  All of the drugs that were developed actually enhanced cholesterol synthesis. 
D)  None of the drugs that were developed could survive the acid conditions in the stomach. 
E)  These drugs caused untreatable gall stones.

Question 5

The most notable structural feature of penicillin is a four-membered ring referred to as a ______________ ring.

Accepted Answer

The answer of The most notable structural feature of penicillin...

Question 6

Thiopurines such as 6-thioguanine are used to treat immune disorders and leukemia. Some individuals who are treated show signs of toxicity at doses well tolerated by most patients. Explain the reason for this toxicity.

Accepted Answer

These differences are due to rare variat

Question 7

Which of the following enzymes is associated with the inflammatory response?

Accepted Answer

A)  phosphodiesterase 5 
B)  HMG-CoA reductase 
C)  $\beta$-lactamase 
D)  cyclooxygenase 2 
E)  None of the answers is correct. 
A)  phosphodiesterase 5 
B)  HMG-CoA reductase 
C)  $\beta$-lactamase 
D)  cyclooxygenase 2 
E)  None of the answers is correct.

Question 8

What set of "rules" gives a general indication of the bioavailability of a drug?

Accepted Answer

A)  Lipovec 
B)  Lipper 
C)  Lippincott 
D)  Lipinski 
E)  Lipkowicz 
A)  Lipovec 
B)  Lipper 
C)  Lippincott 
D)  Lipinski 
E)  Lipkowicz

Question 9

What compound is increased by the action of Sildenafil (Viagra)?

Accepted Answer

A)  GTP 
B)  ATP 
C)  AMP 
D)  cAMP 
E)  cGMP 
A)  GTP 
B)  ATP 
C)  AMP 
D)  cAMP 
E)  cGMP

Question 10

Cyclooxygenase 2 is expressed primarily as part of the inflammatory response, whereas cyclooxygenase 1 is expressed more generally. Celecoxib (Celebrex) was designed to target COX2 and is used to reduce inflammation due to arthritis. What structural feature of Celecoxib (Celebrex) makes this drug more selective for COX2 instead of COX1?

Accepted Answer

X-ray crystallography of COX2 revealed a

Question 11

Who is credited with the discovery of penicillin?

Accepted Answer

A)  Louis Pasteur 
B)  Alexander Fleming 
C)  Selman Waksman 
D)  Paul Ehrlich 
E)  Gerhard Domagk 
A)  Louis Pasteur 
B)  Alexander Fleming 
C)  Selman Waksman 
D)  Paul Ehrlich 
E)  Gerhard Domagk

Question 12

Which of the following properties affects the effective concentration of a drug at the target site?

Accepted Answer

A)  the rate of absorption of the drug 
B)  the extent of distribution or compartmentalization of the drug 
C)  the efficiency of metabolism of the drug 
D)  the ease of excretion of the drug and/or its metabolites 
E)  All of the answers are correct. 
A)  the rate of absorption of the drug 
B)  the extent of distribution or compartmentalization of the drug 
C)  the efficiency of metabolism of the drug 
D)  the ease of excretion of the drug and/or its metabolites 
E)  All of the answers are correct.

Question 13

) What type of bond is used to link a glucuronic acid group to a xenobiotic?

Accepted Answer

A)  eEster 
B)  gGlycosidic 
C)  aAmide 
D)  pPhosphoester 
E)  tThioether 
A)  eEster 
B)  gGlycosidic 
C)  aAmide 
D)  pPhosphoester 
E)  tThioether

Question 14

Kd corresponds to the concentration of ligand, at which ______________ (fraction?) of the receptors are bound to ligand.

Accepted Answer

Question 15

Successful drugs have been discovered by which of the following methods?

Accepted Answer

A)  chance observation of a beneficial, though unplanned, physiological effect 
B)  screening natural products with interesting activities 
C)  combinatorial chemical synthesis of large collections of chemically related compounds for screening 
D)  if the structure of the target is known, computer-aided design of compounds that might bind to the target 
E)  All of the answers are correct. 
A)  chance observation of a beneficial, though unplanned, physiological effect 
B)  screening natural products with interesting activities 
C)  combinatorial chemical synthesis of large collections of chemically related compounds for screening 
D)  if the structure of the target is known, computer-aided design of compounds that might bind to the target 
E)  All of the answers are correct.

Question 16

Briefly describe the factors that will determine the concentration of a drug at the target site in the body.

Accepted Answer

This answer is related to Figure 36.6 an

Question 17

Elevated doses of acetaminophen are toxic because an oxidized metabolite reacts with and depletes which of the following compounds that normally protects the liver and other vital organs?

Accepted Answer

A)  glutathione 
B)  cGMP 
C)  plasma albumin 
D)  vyclooxygenase I 
E)  cytochrome P450 
A)  glutathione 
B)  cGMP 
C)  plasma albumin 
D)  vyclooxygenase I 
E)  cytochrome P450

Question 18

What method, employed in combinatorial chemistry, begins by dividing the starting scaffold into a number of sets?

Accepted Answer

A)  rational drug design 
B)  solid phase synthesis 
C)  split pool synthesis 
D)  high-throughput screening 
E)  None of the answers is correct. 
A)  rational drug design 
B)  solid phase synthesis 
C)  split pool synthesis 
D)  high-throughput screening 
E)  None of the answers is correct.

Question 19

Thiopurine drugs, such as 6-thioguanine, are toxic to some individuals because they have a genetic variation of the enzyme _________________________.

Accepted Answer

thiopurine

Question 20

A compound that inhibits HMG-CoA reductase has potential use as a drug that

Accepted Answer

A)  reduces inflammation and can be used to treat arthritis. 
B)  reduces stomach acid production and can be used to treat ulcers. 
C)  reduces blood cholesterol and can be used to treat atherosclerosis. 
D)  increases the concentration of cGMP and can be used to treat erectile dysfunction. 
E)  increases dopamine and can be used to treat schizophrenia. 
A)  reduces inflammation and can be used to treat arthritis. 
B)  reduces stomach acid production and can be used to treat ulcers. 
C)  reduces blood cholesterol and can be used to treat atherosclerosis. 
D)  increases the concentration of cGMP and can be used to treat erectile dysfunction. 
E)  increases dopamine and can be used to treat schizophrenia.

Exam 36: Drug Development

Which of the following class of drugs is a common treatment for hypertension?

Describe how certain bacteria can development resistance to penicillin.

How is genomic information used to develop new drugs?

First attempts to develop cholesterol-lowering drugs targeted the later steps in cholesterol biosynthesis. Why did this strategy have to be abandoned?

The most notable structural feature of penicillin is a four-membered ring referred to as a ______________ ring.

Thiopurines such as 6-thioguanine are used to treat immune disorders and leukemia. Some individuals who are treated show signs of toxicity at doses well tolerated by most patients. Explain the reason for this toxicity.

Which of the following enzymes is associated with the inflammatory response?

What set of "rules" gives a general indication of the bioavailability of a drug?

What compound is increased by the action of Sildenafil (Viagra)?

Who is credited with the discovery of penicillin?

Which of the following properties affects the effective concentration of a drug at the target site?

) What type of bond is used to link a glucuronic acid group to a xenobiotic?

Kd corresponds to the concentration of ligand, at which ______________ (fraction?) of the receptors are bound to ligand.

Successful drugs have been discovered by which of the following methods?

Briefly describe the factors that will determine the concentration of a drug at the target site in the body.

Elevated doses of acetaminophen are toxic because an oxidized metabolite reacts with and depletes which of the following compounds that normally protects the liver and other vital organs?

What method, employed in combinatorial chemistry, begins by dividing the starting scaffold into a number of sets?

Thiopurine drugs, such as 6-thioguanine, are toxic to some individuals because they have a genetic variation of the enzyme _________________________.

A compound that inhibits HMG-CoA reductase has potential use as a drug that

Biochemistry: an Evolving Science

Protein Composition and Structure

Exploring Proteins and Proteomes

DNA, RNA, and the Flow of Genetic Information

Exploring Genes and Genomes

Exploring Evolution and Bioinformatics

Hemoglobin: a Portrait of a Protein in Action

Enzymes: Basic Concepts and Kinetics

Oxidative Phosphorylation

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Lipids and Cell Membranes

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Signal-Transduction Pathways

Metabolism: Basic Concepts and Design

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The Citric Acid Cycle

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K_d corresponds to the concentration of ligand, at which ______________ (fraction?) of the receptors are bound to ligand.